PF-04634817


Catalog No. Size PriceQuantity
M21127-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

PF-0463481 is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy.

Product information

CAS Number: 1228111-63-4

Molecular Weight: 511.58

Formula: C25H36F3N5O3

Chemical Name: (3S,4S)-3-methoxy-N-[(1R,3S)-3-(propan-2-yl)-3-[(1S,4S)-5-[6-(trifluoromethyl)pyrimidin-4-yl]-2,5-diazabicyclo[2.2.1]heptane-2-carbonyl]cyclopentyl]oxan-4-amine

Smiles: CC(C)[C@]1(C[C@@H](CC1)N[C@H]1CCOC[C@H]1OC)C(=O)N1C[C@@H]2C[C@H]1CN2C1C=C(N=CN=1)C(F)(F)F

InChiKey: MCRWZBYTLVCCJJ-DKALBXGISA-N

InChi: InChI=1S/C25H36F3N5O3/c1-15(2)24(6-4-16(10-24)31-19-5-7-36-13-20(19)35-3)23(34)33-12-17-8-18(33)11-32(17)22-9-21(25(26,27)28)29-14-30-22/h9,14-20,31H,4-8,10-13H2,1-3H3/t16-,17+,18+,19+,20-,24+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (97.74 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

PF-04634817 (oral administration; 30 mg/kg; once daily; 31 days intervention (weeks 2-15 after Streptozotocin)) intervention at the onset of diabetes (week 2) has no impact on the fasting blood glucose levels in diabetic Nos3-/- 221 mice. The development of diabetes results in a marked increase in the levels of glycated haemoglobin (HbA1c) in Nos3-/- mice. Early intervention with PF-04634817 induces an additional increase in glycated hemoglobin (HbA1c) levels.

Products are for research use only. Not for human use.

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